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    Hydrazide-Bridged Pyridazines for Cholinesterase Inhibitors: Synthesis, Characterizations, In Silico, and In Vitro Evaluation
    (Wiley-V C H Verlag Gmbh, 2024) Gursoy, Sule; Onel, Gulce Taskor; Turkmenoglu, Burcin; Merde, Irem Bozbey; Dilek, Esra; Hepokur, Ceylan; Algul, Oztekin
    In this study, we investigate the inhibitory potential of a series of hydrazide derivatives bearing different substituents with the pyridazine structure (5 a-i and 6 a-f) against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using a modified Ellman's method. The inhibitory profiles of the synthesized compounds were assessed by comparing their IC50 and Ki values. Our results demonstrate that all the compounds exhibit significant inhibitory activity against both AChE and BChE when compared to the reference compound, tacrine. Particularly, compound 6 a exhibited the highest activity against Electrophorus electricus AChE (EeAChE) with a Ki value of 3.26 nM, while compound 5 a displayed the most potent inhibition against equine BChE (eqBChE) with a Ki value of 0.94 nM. The compounds did not possess significant cytotoxicity action using the MTT assay on the cancer cell lines. The DPPH assays revealed that all the compounds have moderate antioxidant activities. Furthermore, molecular docking studies provided valuable insights into the interaction mechanisms of these compounds within the active sites of AChE and BChE crystal structures (PDB ID: 4EY7 and 4BDS, respectively). The above results indicated that the pyridazine-based compounds were a promising functional agent for the treatment of Alzheimer's disease. This study reveals the potential of hydrazide derivatives, each with distinct substituents on the pyridazine structure, as potent enzyme inhibitors (AChE and BChE) with antioxidant properties. The provided structural insights, inhibitory profiles, and molecular docking results emphasize their therapeutic potential for neurological disorders. These findings lay the groundwork for subsequent exploration and drug development within the domain of pyridazine compounds. image
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    Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme
    (Marmara Univ, 2022) Bozbey, Irem; Onel, Gulce Taskor; Turkmenoglu, Burcin; Gursoy, Sule; Dilek, Esra; Ergun, Muhammed; Ozcelik, Azime Berna
    Alzheimer's disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 3(2H)pyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants (Ki) of the compounds against the AChE enzyme ranged from 2.35 +/- 0.18 to 5.15 +/- 0.46 mu M. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35 +/- 0.18 mu M. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure (PDB ID:4M0E).